Alprazolam

General characteristics. Structure:

Active ingredient: 1,0 mg or 0,25 mg of an alprazolam.

Excipients: lactoses monohydrate (sugar milk); potato starch; povidone low-molecular (PVP low-molecular medical 12600±2700); stearate magnesium monohydrate (magnesium stearate).

Anxiolytic drug with some antidepressive, somnolent and anticonvulsant effect.

Pharmacological properties:

Pharmacodynamics. Anxiolytic means (tranquilizer) derivative of triazolo-benzodiazepine. Renders anxiolytic, sedative, somnolent, anticonvulsant, central myorelaxation action. The mechanism of action consists in strengthening of brake influence of endogenous GABA in TsNS due to increase in sensitivity of GABA receptors to a mediator as a result of stimulation of the benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating reticular formation of a brainstem and internuncial neurons of side horns of a spinal cord; reduces excitability of subcrustal structures of a brain (limbic system, a thalamus, a hypothalamus), brakes polisinaptichesky spinal reflexes.

Indications to use:

The alarming states, neurosises which are followed by feeling of alarm, danger, concern, tension, deterioration in a dream, irritability, and also somatic disturbances; the mixed alarming depressions; the neurotic reactive depressions which are followed by decrease in mood, loss of interest to surrounding concern, loss of a dream, a loss of appetite, somatic disturbances; the alarming states and neurotic depressions which developed against the background of somatopathies; panic frustration in a combination and without phobia symptoms.

Route of administration and doses:

Individual. It is recommended to use minimal effective doses. The dose is korrigirut in the course of treatment depending on the reached effect and portability. In need of increase in a dose it should be increased gradually, in the beginning in evening, and then in day reception.

The initial dose makes 250-500 mkg of 3 times/days, if necessary perhaps gradual increase up to 4.5 mg/days.

For the elderly or weakened patients the initial dose makes 250 mkg of 2-3 times/days, maintenance doses - 500-750 mkg/days, if necessary taking into account portability the dose can be increased.

Cancellation or dose decline of an alprazolam should be carried out gradually, lowering a daily dose no more than by 500 mkg each 3 days; slower cancellation can sometimes be required.

Features of use:

At endogenous depressions alprazola can apply in a combination with antidepressants. At use of an alprazolam for patients with a depression cases of development of a hypomaniacal and maniacal state are noted.

With care alprazola should apply at patients with abnormal liver functions and/or kidneys.

At the patients who were earlier not accepting the medicines influencing TsNS, to alprazola it is effective in lower doses, in comparison with patients who received antidepressants, anxiolytics or suffering from an alcoholism.

At prolonged use in high doses development of accustoming and formation of medicinal dependence, especially at the patients inclined to abuse of medicines is possible.

At a bystry dose decline or sharp cancellation of an alprazolam the withdrawal which symptoms can fluctuate from a small dysphoria and sleeplessness to a heavy syndrome with spasms in a stomach and skeletal muscles, vomiting, sweating strengthening, a tremor and spasms is observed. The withdrawal meets at persons more often, is long (more than 8-12 weeks) receiving to alprazola.

It is not necessary to apply along with alprazolamy other tranquilizers.

Safety of use of an alprazolam for children and teenagers aged up to 18 years is not established. Children, especially at younger age, are very sensitive to the oppressing effect of benzodiazepines on TsNS.

During treatment not to allow alcohol intake.

During treatment it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and speed of psychomotor reactions (driving of vehicles or work with mechanisms).

Alprazolam has toxic effect on a fruit and increases risk of development of inborn defects at use in the I trimester of pregnancy. Constant use during pregnancy can result in physical dependence with development of a withdrawal in the newborn. Inclusion in therapeutic doses in later durations of gestation can cause oppression of TsNS of the newborn. Use just before childbirth or at the time of delivery can cause in the newborn respiratory depression, decrease in a muscle tone, hypotension, a hypothermia and the weak act of suction (a syndrome of sluggish suction of the newborn).

Release of benzodiazepines with breast milk is possible that can cause drowsiness in the newborn and complicate feeding.

In pilot studies it is shown that and its metabolites are allocated to alprazola with breast milk.

For the elderly or weakened patients the initial dose makes 250 mkg of 2-3 times/days, maintenance doses - 500-750 mkg/days, if necessary taking into account portability the dose can be increased.

With care alprazola should apply at patients with abnormal liver functions.

Side effects:

From TsNS: in an initiation of treatment (especially at patients of advanced age) drowsiness, feeling of fatigue, dizziness, decline in the ability to concentration of attention, an ataxy, a disorientation, instability of gait, delay of mental and motor reactions; seldom - a headache, euphoria, a depression, a tremor, decrease in memory, a lack of coordination of movements, depression of mood, confusion of consciousness, dystonic extrapyramidal reactions (the uncontrollable movements, including an eye), weakness, a myasthenia, a dysarthtia; in some cases - paradoxical reactions (aggressive flashes, confusion of consciousness, psychomotor excitement, fear, suicide bent, a muscular spasm, hallucinations, excitement, irritability, uneasiness, sleeplessness).

From the alimentary system: are possible dryness in a mouth or hypersalivation, heartburn, nausea, vomiting, a loss of appetite, locks or diarrhea, an abnormal liver function, increase in activity of hepatic transaminases and ShchF, jaundice.

From system of a hemopoiesis: the leukopenia, a neutropenia, an agranulocytosis (a fever, a hyperthermia, pharyngalgias, excessive fatigue or weakness), anemia, thrombocytopenia are possible.

From an urinary system: the urine incontience, an ischuria, a renal failure, decrease or increase in a libido, a dysmenorrhea are possible.

From endocrine system: change of body weight, disturbance of a libido, disturbance of a menstrual cycle are possible.

From cardiovascular system: decrease in the ABP, tachycardia is possible.

Allergic reactions: skin rash, an itch are possible.

Interaction with other medicines:

At simultaneous use psychotropic, anticonvulsant, means and ethanol strengthening of the oppressing action of an alprazolam on TsNS is observed.

At simultaneous use blockers histamine H2 receptors reduce clearance of an alprazolam and strengthen the oppressing action of an alprazolam on TsNS; antibiotics from group of macroleads - reduce clearance of an alprazolam.

At simultaneous use hormonal contraceptives for intake increase T1/2 of an alprazolam.

At simultaneous use of an alprazolam with dextropropoxyphene more expressed oppression of TsNS, than in a combination with other benzodiazepines since increase in concentration of an alprazolam in a blood plasma is possible is observed.

The concomitant use of digoxin increases risk of development of intoxication by cardiac glycosides.

Alprazolam increases concentration of Imipraminum in a blood plasma.

At simultaneous use итраконазол, кетоконазол strengthen effects of an alprazolam.

At simultaneous use of a paroksetin strengthening of effects of an alprazolam caused by oppression of his metabolism is possible.

Fluvoksamin increases concentration of an alprazolam in a blood plasma and risk of development of its side effects.

At simultaneous use of fluoxetine increase in concentration of an alprazolam in a blood plasma owing to reduction of his metabolism and clearance under the influence of fluoxetine is possible that is followed by psychomotor disturbances.

It is impossible to exclude a possibility of strengthening of action of an alprazolam at simultaneous use with erythromycin.

Contraindications:

Coma, shock, myasthenia, closed-angle glaucoma (bad attack or predisposition), acute alcoholic poisonings (with weakening of the vital functions), opioid analgetics, hypnotic drugs and psychotropic drugs, chronic obstructive respiratory diseases with initial manifestations of respiratory insufficiency, acute respiratory insufficiency, a heavy depression (suicide bents), pregnancy (especially the I trimester can be shown), the lactation period, children's and teenage age up to 18 years, hypersensitivity to benzodiazepines.

Overdose:

At administration of drug Alprazolam in the doses considerably exceeding recommended (more than 500 mg at one time) at patients development of confusion of consciousness, drowsiness, deterioration in coordination of movements, a nystagmus, decrease in reflexes, alalias, arterial hypertension, and also coma is possible.

At overdose of an alprazolam the gastric lavage and purpose of enterosorbentny means is shown (for the purpose of decrease in absorption of an alprazolam). If necessary hold the events and therapy directed to maintenance of function of cardiovascular and respiratory system. When performing therapy of overdose in the conditions of a hospital introduction of a flumazenil is shown.

Storage conditions:

The list III of the list of the drugs, psychotropic substances and their precursors which are subject to control in the Russian Federation. To store in the place protected from light at a temperature not above 30 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 1,0 mg. 50 pieces - banks of dark glass (1) - a pack cardboard.
10 pieces - planimetric strip packagings (5) - packs cardboard.

Tablets on 0,25 mkg. 50 pieces - banks of dark glass (1) - a pack cardboard.